Size | Price | Stock | Qty |
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1mg |
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5mg |
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Other Sizes |
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Targets |
GR[1]
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ln Vitro |
Dazucorilant functions as a complete antagonist in human hepatocytes or HepG2 human cells since it can both provide non-measurable agonist activity in the absence of dexamethasone and stop the rise in TAT activity brought on by dexamethasone[3].
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ln Vivo |
Dazucorilant (30 mg/kg/day; SC) causes mice to exhibit glial reactivity, down-regulated proinflammatory mediators, and motoneurons with abnormalities reversed[1]. At a dose of 10 mg/kg, dazucorilant (5, 10 or 20 mg/kg; ip) improves cognitive function by reversing the production of amyloid-β peptides in the hippocampus, as well as neuroinflammation and apoptotic processes. It also restores the levels of synaptic markers in the hippocampus and baseline plasma levels of glucocorticoids.
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Animal Protocol |
Animal/Disease Models: Wobbler mice (five-month-old)[1]
Doses: 30 mg/kg/day Route of Administration: Sc Experimental Results: Wobbler mice demonstrated reversed abnormalities of motoneurons and down-regulated proinflammatory mediators and glial reactivity. Animal/Disease Models: Adult SD male rats[2] Doses: 5, 10 or 20 mg /kg Route of Administration: Ip Experimental Results: Reversed hippocampal amyloid-β peptide generation, neuroinflammation and apoptotic processes, restored the hippocampal levels of synaptic markers, reestablished basal plasma levels of glucocorticoids and improved cognitive function at a dose of 10 mg/kg. |
References |
[1]. Meyer M, et al. The Selective Glucocorticoid Receptor Modulator Cort 113176 Reduces Neurodegeneration and Neuroinflammation in Wobbler Mice Spinal Cord. Neuroscience. 2018;384:384-396.
[2]. Pineau F, et al. New selective glucocorticoid receptor modulators reverse amyloid-β peptide-induced hippocampus toxicity. Neurobiol Aging. 2016;45:109-122. [3]. Canet G, et al. Central Role of Glucocorticoid Receptors in Alzheimer's Disease and Depression. Front Neurosci. 2018;12:739. Published 2018 Oct 16. |
Molecular Formula |
C29H22F4N4O3S
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Molecular Weight |
582.57
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CAS # |
1496508-34-9
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SMILES |
S(C1C([H])=C([H])C(C(F)(F)F)=C([H])C=1[H])(N1C([H])([H])C([H])([H])C2=C([H])C3=C(C([H])=NN3C3C([H])=C([H])C(=C([H])C=3[H])F)C([H])([H])[C@]2(C(C2=C([H])C([H])=C([H])C([H])=N2)=O)C1([H])[H])(=O)=O
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7165 mL | 8.5827 mL | 17.1653 mL | |
5 mM | 0.3433 mL | 1.7165 mL | 3.4331 mL | |
10 mM | 0.1717 mL | 0.8583 mL | 1.7165 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.